221445-27-8Relevant articles and documents
Synthesis, antiepileptic effects, and structure-activity relationships of α-asarone derivatives: In vitro and in vivo neuroprotective effect of selected derivatives
Zhang, Jian,Mu, Keman,Yang, Peng,Feng, Xinqian,Zhang, Di,Fan, Xiangyu,Wang, Qiantao,Mao, Shengjun
, (2021/08/03)
In the present study, we compared the antiepileptic effects of α-asarone derivatives to explore their structure-activity relationships using the PTZ-induced seizure model. Our research revealed that electron-donating methoxy groups in the 3,4,5-position on phenyl ring increased antiepileptic potency but the placement of other groups at different positions decreased activity. Besides, in allyl moiety, the optimal activity was reached with either an allyl or a 1-butenyl group in conjugation with the benzene ring. The compounds 5 and 19 exerted better neuroprotective effects against epilepsy in vitro (cell) and in vivo (mouse) models. This study provides valuable data for further exploration and application of these compounds as potential anti-seizure medicines.
Phenol-Substituted Tetrapyrazinoporphyrazines: pH-Dependent Fluorescence in Basic Media
Novakova, Veronika,Lásková, Miroslava,Vav?i?ková, Hana,Zimcik, Petr
supporting information, p. 14382 - 14392 (2015/10/05)
Tetrapyrazinoporphyrazines (TPyzPzs) bearing one, two, four or eight 3,5-di(tert-butyl)-4-hydroxyphenol moieties were synthesized as zinc(II) complexes and metal-free derivatives. The deprotonation of the phenol using tetrabutylammonium hydroxide induced the formation of a strong donor for intramolecular charge transfer that switched OFF the red fluorescence (λF660 nm) of the parent zinc TPyzPzs. The changes were fully reversible for TPyzPzs with one to four phenolic moieties, and an irreversible modification was observed for TPyzPzs substituted with eight phenols. The sensors were anchored to lipophilic particles in water, and a pKa approximately 12.5-12.7 was determined for the phenolic hydroxyl based on fluorescence changes in different buffers. In addition, a novel concept for fluorescence OFF-ON-OFF switching in metal-free TPyzPzs bearing phenolic moieties upon addition of specific amounts of base was demonstrated.
Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series
Song, Yuntao,Connor, David T.,Doubleday, Robert,Sorenson, Roderick J.,Sercel, Anthony D.,Unangst, Paul C.,Roth, Bruce D.,Gilbertsen, Richard B.,Chan, Kam,Schrier, Denis J.,Guglietta, Antonio,Bornemeier, Dirk A.,Dyer, Richard D.
, p. 1151 - 1160 (2007/10/03)
Selective cyclooxygenase-2 (COX-2) inhibitors have been shown to be potent antiinflammatory agents with fewer side effects than currently marketed nonsteroidal antiinflammatory drugs (NSAIDs). Initial mass screening and subsequent structure-activity relat